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1.
Nanomaterials (Basel) ; 13(11)2023 May 26.
Artículo en Inglés | MEDLINE | ID: mdl-37299646

RESUMEN

Porous carbon materials have demonstrated exceptional performance in various energy and environment-related applications. Recently, research on supercapacitors has been steadily increasing, and porous carbon materials have emerged as the most significant electrode material for supercapacitors. Nonetheless, the high cost and potential for environmental pollution associated with the preparation process of porous carbon materials remain significant issues. This paper presents an overview of common methods for preparing porous carbon materials, including the carbon-activation method, hard-templating method, soft-templating method, sacrificial-templating method, and self-templating method. Additionally, we also review several emerging methods for the preparation of porous carbon materials, such as copolymer pyrolysis, carbohydrate self-activation, and laser scribing. We then categorise porous carbons based on their pore sizes and the presence or absence of heteroatom doping. Finally, we provide an overview of recent applications of porous carbon materials as electrodes for supercapacitors.

2.
Chem Biol Drug Des ; 87(3): 444-54, 2016 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-26518975

RESUMEN

Based on our previous work, seven N(5) -substituted 8,10-dideazatetrahydrofolate analogues and one 8-deazatetrahydrofolate analogue were designed and synthesized as human dihydrofolate reductase (hDHFR) inhibitors. All compounds were assayed versus DHFR and five different cancer cell lines. The biological assay indicated that replacing N(10) with carbon would significantly increase inhibitory activities against DHFR and cytotoxicities against cancer cell lines. Compound 19a with 4-amino and N(5) -formyl showed great antitumour activities against HL-60, Bel-7402 and BGC823 which were much better than MTX.


Asunto(s)
Antineoplásicos/síntesis química , Antineoplásicos/farmacología , Antagonistas del Ácido Fólico/síntesis química , Antagonistas del Ácido Fólico/farmacología , Espectroscopía de Resonancia Magnética , Espectrometría de Masa por Ionización de Electrospray
3.
Eur J Med Chem ; 58: 228-36, 2012 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-23124219

RESUMEN

A number of 8-deazatetrahydrofolates bearing electrophilic groups on N(5) were designed and synthesized based on the action mechanism of methionine synthase, and their biological activities were investigated as well. Compounds (11b, 12b and 16) showed the most active against methionine synthase (IC(50): 8.11 µM, 1.73 µM, 1.43 µM). In addition, the cytotoxicity to human tumor cell lines and dihydrofolate reductase (DHFR) inhibition by target compounds were evaluated.


Asunto(s)
5-Metiltetrahidrofolato-Homocisteína S-Metiltransferasa/antagonistas & inhibidores , Antineoplásicos/farmacología , Diseño de Fármacos , Inhibidores Enzimáticos/farmacología , Tetrahidrofolatos/farmacología , 5-Metiltetrahidrofolato-Homocisteína S-Metiltransferasa/metabolismo , Antineoplásicos/síntesis química , Antineoplásicos/química , Muerte Celular/efectos de los fármacos , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Ensayos de Selección de Medicamentos Antitumorales , Inhibidores Enzimáticos/síntesis química , Inhibidores Enzimáticos/química , Células HeLa , Humanos , Modelos Moleculares , Estructura Molecular , Relación Estructura-Actividad , Tetrahidrofolato Deshidrogenasa/metabolismo , Tetrahidrofolatos/síntesis química , Tetrahidrofolatos/química
4.
Molecules ; 17(5): 5604-14, 2012 May 10.
Artículo en Inglés | MEDLINE | ID: mdl-22576230

RESUMEN

An efficient method for the construction of the tetrahydrofolate skeleton is described. Starting from pterin analogues and aromatic amines, 8-deaza-5,6,7,8-tetrahydroaminopterin derivatives and the heterocyclic benzoyl isosteres were synthesized via a novel aziridine intermediate. Following this method, the byproducts of carbon-nitrogen bond hydrogenolysis in traditional synthetic strategy can be completely avoided.


Asunto(s)
Aminopterina/síntesis química , Aziridinas/química , Aminopterina/análogos & derivados , Carbono/química , Hidrogenación , Espectroscopía de Resonancia Magnética , Nitrógeno/química , Tetrahidrofolatos/química
5.
Eur J Med Chem ; 44(2): 764-71, 2009 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-18555562

RESUMEN

We report, for the first time, the synthesis and biological activities of 8-deaza-5,6,7,8-tetrahydroaminopterin 9, and the 5-substituted and 5,10-disubstituted analogues 11, 13, 15, and 17. The analogues were obtained from key compound diethyl 8-deaza-5,6,7,8-tetrahydroaminopterin 8 following the catalytic reduction of the pyridine ring of diethyl 8-deaza aminopterin 5. The five novel 8-deaza-5,6,7,8-tetrahydroaminopterin derivatives were assayed in vitro for their cytotoxicity on BGC-823, HL-60, Bel-7402 and Hela tumor cell lines, and inhibition on recombinant human dihydrofolate reductase (DHFR), among which the most potent molecule (compound 9) was about 4- to 10-fold poorer than MTX on the four kinds of tumor cell lines, and its effect on DHFR was about 17-fold poorer than MTX. The docking studies were followed to explain the biological testing results.


Asunto(s)
Aminopterina/análogos & derivados , Antagonistas del Ácido Fólico/síntesis química , Aminopterina/síntesis química , Aminopterina/farmacología , Línea Celular Tumoral , Simulación por Computador , Diseño de Fármacos , Ensayos de Selección de Medicamentos Antitumorales , Inhibidores Enzimáticos/síntesis química , Inhibidores Enzimáticos/farmacología , Antagonistas del Ácido Fólico/farmacología , Humanos , Unión Proteica , Relación Estructura-Actividad , Tetrahidrofolato Deshidrogenasa/efectos de los fármacos , Tetrahidrofolato Deshidrogenasa/metabolismo
6.
Beijing Da Xue Xue Bao Yi Xue Ban ; 40(4): 443-5, 2008 Aug 18.
Artículo en Chino | MEDLINE | ID: mdl-18677396

RESUMEN

OBJECTIVE: To find a best synthesis method of diethyl N-[p-(methylamino)benzoyl]-L-glutamate(1). METHODS: Using diethyl N-(p- aminobenzoyl)-L-glutamate (2) as a starting material via a one-pot process of benzylation and methylation, the diethyl N-[p-(methylamino)benzoyl ]-L-glutamate (3) is prepared in high yield. Then compound 1 was conveniently obtained from debenzylation of compound 3 by Pd/C. RESULTS: The target compound was obtained through 2-step reaction in 88% overall yield in only 6 h, and its structure was identified by 1HNMR and MS. CONCLUSION: It is a convenient and efficient method of preparation of diethyl N-[p-(methylamino)benzoyl]-L-glutamate.


Asunto(s)
Glutamatos/química , Glutamatos/síntesis química
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